Chemical: Drug

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The table below contains information about pharmacogenomic variants on PharmGKB. Please follow the link in the "Variant" column for more information about a particular variant. Each link in the "Variant" column leads to the corresponding PharmGKB Variant Page. The Variant Page contains summary data, including PharmGKB manually curated information about variant-drug pairs based on individual PubMed publications. The PMIDs for these PubMed publications can be found on the Variant Page.

The tags in the first column of the table indicate what type of information can be found on the corresponding Variant Page.

Links in the "Gene" column lead to PharmGKB Gene Pages.

List of all variant annotations for tiludronate

Gene ? Variant?
Alternate Names ? Chemicals ? Alleles ?
(+ chr strand)
Function ? Amino Acid?
No VIP available CA No Variant Annotations available
rs16944 NC_000002.11:g.113594867A>G, NC_000002.12:g.112837290A>G, NG_008851.1:g.4490T>C, NM_000576.2:c.-598T>C, XM_006712496.1:c.-1552T>C, rs3827762
A > G
Alleles, Functions, and Amino Acid Translations are all sourced from dbSNP 147


Generic Names
  • Acide tiludronique [INN-French]
  • Acido tiludronico [INN-Spanish]
  • Acidum tiludronicum [INN-Latin]
  • Tiludronate disodium
  • Tiludronic Acid Disodium Salt
  • Tiludronic acid
Trade Names
  • Skelid
Brand Mixture Names

PharmGKB Accession Id





Tiludronate is a bisphosphonate characterized by a (4-chlorophenylthio) group on the carbon atom of the basic P-C-P structure common to all bisphosphonates.

Source: Drug Bank


For treatment of Paget's disease of bone (osteitis deformans).

Source: Drug Bank

Other Vocabularies

Information pulled from DrugBank has not been reviewed by PharmGKB.

Pharmacology, Interactions, and Contraindications

Mechanism of Action

The bisphosphonate group binds strongly to the bone mineral, hydroxyapatite. This explains the specific pharmacological action of these compounds on mineralized tissues, especially bone. _In vitro_ studies indicate that tiludronate acts primarily on bone through a mechanism that involves inhibition of osteoclastic activity with a probable reduction in the enzymatic and transport processes that lead to resorption of the mineralized matrix. Bone resorption occurs following recruitment, activation, and polarization of osteoclasts. Tiludronate appears to inhibit osteoclasts by at least two mechanisms: disruption of the cytoskeletal ring structure, possibly by inhibition of protein-tyrosine-phosphatase, thus leading to detachment of osteoclasts from the bone surface and the inhibition of the osteoclastic proton pump.

Source: Drug Bank


Tiludronate is a first generation (non-nitrogenous) bisphosphonate in the same family as etidronate and clodronate. Tiludronate affects calcium metabolism and inhibits bone resorption and soft tissue calcification. Of the tiludronate that is resorbed (from oral preparation) or infused (for intravenous drugs), about 50% is excreted unchanged by the kidney. The remainder has a very high affinity for bone tissue, and is rapidly absorbed onto the bone surface.

Source: Drug Bank

Food Interaction

Do not take aluminum or magnesium-containing antacids within 2 hours of taking tiludronate.|Take on an empty stomach (at least 2 hours before or after meals) with a full glass of plain water. Other beverages may reduce drug absorption.

Source: Drug Bank

Absorption, Distribution, Metabolism, Elimination & Toxicity


In vitro, tiludronic acid is not metabolized in human liver microsomes and hepatocytes. There is no evidence that tiludronate is metabolized in humans.

Source: Drug Bank

Protein Binding

Approximately 90% bound to human serum protein (mainly albumin) at plasma concentrations between 1 and 10 mg/L.

Source: Drug Bank


The mean oral bioavailability in healthy male subjects is 6% after an oral dose equivalent to 400 mg tiludronic acid administered after an overnight fast and 4 hours before a standard breakfast. In single-dose studies, bioavailability was reduced by 90% when an oral dose equivalent to 400 mg tiludronic acid was administered with, or 2 hours after, a standard breakfast compared to the same dose administered after an overnight fast and 4 hours before a standard breakfast.

Source: Drug Bank


Half-life in healthy subjects is 50 hours following administration of a 400 mg single oral dose. Half-life in pagetic patients is about 150 hours following administration of 400 mg tiludronate a day for 12 days. In patients with renal insufficiency (creatinine clearance between 11 and 18 mL per minute [mL/min]), half-life is 205 hours from plasma after administration of a single, oral dose equivalent to 400 mg tiludronate.

Source: Drug Bank


Based on the known action of tiludronate, hypocalcemia is a potential consequence of overdose. In one patient with hypercalcemia of malignancy, intravenous administration of high doses (800 mg/day total dose, 6 mg/kg/day for 2 days) was associated with acute renal failure and death.

Source: Drug Bank


* renal cl=10 mL/min [IV administration of 20-mg dose]

Source: Drug Bank

Route of Elimination

The principal route of elimination of tiludronic acid is in the urine.

Source: Drug Bank

Chemical Properties

Chemical Formula


Source: Drug Bank

Isomeric SMILES


Source: Drug Bank


Source: Drug Bank

Canonical SMILES


Source: Drug Bank

Average Molecular Weight


Source: Drug Bank

Monoisotopic Molecular Weight


Source: Drug Bank



Source: Drug Bank

InChI String


Source: Drug Bank

Genes that are associated with this drug in PharmGKB's database based on (1) variant annotations, (2) literature review, (3) pathways or (4) information automatically retrieved from DrugBank, depending on the "evidence" and "source" listed below.

Curated Information ?

No Dosing Guideline available No Drug Label available CA No Variant Annotation available No VIP available No VIP available

Drug Targets

Gene Description
ATP6V1A (source: Drug Bank )
PTPN1 (source: Drug Bank )

Drug Interactions

Interaction Description
tiludronate - calcium The divalent cation of oral Calcium Chloride may significantly decrease the absorption of Tiludronate by forming a nonabsorbable chelate. Oral dosing should be separated by at least 2 hours. (source: Drug Bank )
tiludronate - Magnesium The divalent cation of oral Magnesium oxide may significantly decrease the absorption of Tiludronate by forming a nonabsorbable chelate. Oral dosing should be separated by at least 2 hours. (source: Drug Bank )

Curated Information ?

No Dosing Guideline available No Drug Label available CA No Variant Annotation available No VIP available No VIP available
Osteitis Deformans

Relationships from National Drug File - Reference Terminology (NDF-RT)

May Treat
Contraindicated With

Publications related to tiludronate: 1

No Dosing Guideline available No Drug Label available CA No Variant Annotation available No VIP available No VIP available
-511 C/T IL1B gene polymorphism is associated to resistance to bisphosphonates treatment in Paget disease of bone. Bone. 2006. Corral-Gudino Luis, et al. PubMed


Web Resource:
National Drug Code Directory:
KEGG Compound:
PubChem Compound:
PubChem Substance:
FDA Drug Label at DailyMed:

Clinical Trials

These are trials that mention tiludronate and are related to either pharmacogenetics or pharmacogenomics.

No trials loaded.

NURSA Datasets

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No NURSA datasets available.

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Sources for PharmGKB drug information: DrugBank, PubChem.